Drug/Small Molecule:
oxazepam

2D structure

Overview

Generic Names: Oxazipam; Oxozepam; d-Oxazepam hemisuccinate
Trade Names: Adumbran; Ansioxacepam; Anxiolit; Aplakil; Astress; Azutranquil; Bonare; Drimuel; Droxacepam; Durazepam; Enidrel; Hi-Long; Isodin; Lederpam; Limbial; Murelax; Nesontil; Noctazepam; Notaral; Oxa-puren; Oxanid; Pacienx; Praxiten; Propax; Psiquiwas; QUEN; Quilibrex; Rondar; Sedigoa; Serax; Serenal; Serenid; Serenid-D; Serepax; Seresta; Serpax; Sigacalm; Sobril; Tacepam; Tazepam; Uskan; Vaben; Wy-3498 stic; Zaxopam
PharmGKB Accession Id: PA450731

Description

A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia. PubChem (source: Drug Bank)

Indication

For the treatment of anxiety disorders. (source: Drug Bank)

ATC Therapeutic Category

  • N05BA:Benzodiazepine derivatives

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Oxazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation. (source: Drug Bank)

Pharmacology

Oxazepam is a drug which is a benzodiazepine derivative. It possesses relatively weak anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Take with food. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Absorption

Well absorbed from the gastrointestinal tract following oral administration. (source: Drug Bank)

Toxicity

Symptoms of overdose include confusion, drowsiness, and lethargy. (source: Drug Bank)

Isomeric SMILES Code:

c1ccc(cc1)C2=NC(C(=O)Nc3c2cc(cc3)Cl)O (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs1902023 at chr4:69218679
    Study in human liver microsomes from 54 patients, primarily of Caucasian (n=48) descent: D85Y genotype showed a significant effect (p = 0.012) on S-oxazepam glucuronidation with lower median activities in 85Y/Y livers (49 pmol/min/mg protein) compared with 85D/D livers (131 pmol/min/mg), whereas 85D/Y livers were intermediate in activity (65 pmol/min/mg).
    Variant Name:
    D85Y
    Related Drugs:
    oxazepam
    Evidence:
    PMID:15044558
  2. rs1902023 at chr4:69218679
    Risk or phenotype-associated allele(s): T/T . Phenotype: Median oxazepam apparent oral clearance was significantly lower in 85YY subjects (1.62 ml min(-1) kg(-1)) compared with 85DD subjects (3.35 ml min(-1) kg(-1); P= 0.003, Student-Newman-Keuls test), whereas 85DY subjects were intermediate (2.34 ml min(-1) kg(-1); P= 0.018 vs. 85DD, P= 0.034 vs. 85YY). Regression analysis indicated that UGT2B15 D85Y genotype accounted for 34% of interindividual variability. Study size: 30. Study population/ethnicity: healthy male subjects.
    Variant Name:
    291G/T; D85Y
    Related Drugs:
    oxazepam
    Evidence:
    PMID:19916996
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
GABRA1
  •   
  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
GABRB2
  •   
  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
GABRG2
  •   
  • PD
  •   
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  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
UGT1A9
  •   
  •   
  • PK
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Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
UGT2B15
  •   
  •   
  • PK
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
UGT2B17
  •   
  •   
  • PK
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  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
UGT2B7
  •   
  •   
  • PK
  •   
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

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ALB Uncurated Annotation (source: Drug Bank)
GABRA1 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
clozapine Uncurated Annotation Increased risk of toxicity (source: Drug Bank)
mephenytoin Uncurated Annotation Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
phenytoin Uncurated Annotation Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00842
ChEBI ID:
7823
KEGG Compound ID:
C07359
KEGG Drug ID:
D00464
PubChem Compound ID:
4616
PubChem Substance ID:
9563

Common Searches

Search PubMed
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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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